146954-29-2

Upstream product

• 31590-12-2 2-(2-azidophenyl)ethan-1-ol 
• 146954-31-6 N-<2-(o-azidophenyl)ethyl>phthalimide 

Downstream Products

• 1027045-93-7 [2-(2-Azido-phenyl)-ethyl]-[1-(2-azido-phenyl)-meth-(E)-ylidene]-amine 
• 251317-83-6 N-[2-(2-azido-phenyl)-ethyl]-2,2,2-trifluoro-acetamide 
• 1027902-92-6 C₅₂H₄₇N₃P₂ 
• 1027393-43-6 C₅₂H₄₇N₃P₂ 
• 153895-98-8 C₅₁H₄₅N₃P₂ 
• 160060-86-6 C₅₁H₄₃N₃OP₂ 

Relevant academic research and scientific papers

Method for inhibition of HIV related viruses

Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.

Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs

A novel series of potent specific HIV-1 inhibitory compounds is described. The lead compound in the series, N-(2-phenethyl)-N'-(2-thiazolyl)thiourea (1), inhibits HIV-1 RT using rCdG as the template with an IC50 of 0.9 μM. In MT-4 cells, compound 1 inhibits HIV-1 with an ED50 of 1.3 μM. The 50% cytotoxic dose in cell culture is >380 μM. The chemical structure-activity relationship (SAR) was developed by notionally dividing the lead compound in four quadrants. The SAR strategy had two phases. The first phase involved optimization of antiviral activity through independent variation of quadrants 1-4. The second phase involved the preparation of hybrid structures combining the best of these substituents. Further SAR studies and pharmacokinetic considerations led to the identification of N-(2-pyridyl)-N'-(5-bromo-2- pyridyl)-thiourea (62; LY300046 · HCl) as a candidate for clinical evaluation. LY300046 · HCl inhibits HIV-1 RT with an IC50 of 15 nM and in cell culture has an ED50 of 20 nM.

Synthetic Applications of Bis(iminophosphoranes). One-Pot Preparation of Rigid Bicyclic Guanidines

A one-pot synthesis of , , and bicyclic guanidines based on a new method of dihydropyrimido annelation, which involves reaction of bis(iminophosphoranes) with aryl isocyanates or isothiocyanates is described.The method is also applic